Bepotastine tosylate
Based on 1 publication(s) in Google Scholar
Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus.
For research use only. We do not sell to patients.
- CAS No.: 1160415-45-1
- Formula: C28H33ClN2O6S
- Molecular Weight:561.09
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Bepotastine tosylate
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Biological Activity
Description
IC50 & Target
In Vitro
Bepotastine tosylate (10, 100, 1000 µM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 µM[1].
Bepotastine tosylate (50 µM; 1 h) suppresses the expression of NGF mRNA in NHEKs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RPMCs
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Concentration:10, 100, 1000 µM
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Incubation Time:120 min (preincubate)
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Result:Decreased the release of histamine.
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Cell Line:NHEKs
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Concentration:50 µM (preincubation)
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Incubation Time:1 h
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Result:Suppressed the expression of NGF mRNA in NHEKs.
In Vivo
Bepotastine tosylate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control[3].
Bepotastine tosylate (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pigs (6-week-old)[1].
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Dosage:10 g/L (1.0% (w/v)) for 10 µL.
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Administration:Eye drop; 3 times at intervals of 20 min (in one eye)
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Result:Inhibited PAF-induced conjunctival eosinophil infiltration.
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Animal Model:Male BALB/c mice(12-week-old); NC/Nga mice[3].
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Dosage:3, 10 mg/kg
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Administration:Oral administration; once (1 h before induces scratching behavior of Male BALB/c mice).
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Result:Significantly inhibited histamine-mediated scratching behavior in male BALB/c mice.
Significantly suppressed serum LTB 4 levels in NC/Nga mice with a rash.
Chemical Information
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CAS No. 1160415-45-1
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Molecular Weight 561.09
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Formula C28H33ClN2O6S
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SMILES
O=S(C1=CC=C(C)C=C1)(O)=O.O=C(O)CCCN2CCC(CC2)O[C@H](C3=NC=CC=C3)C(C=C4)=CC=C4Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967
Purity & Documentation
References
[1]. Kida T, et al. Bepotastine besilate, a highly selective histamine H(1) receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis models. Exp Eye Res. 2010 Jul;91(1):8 [Content Brief]
[2]. Kamata Y, et al. Bepotastine besilate downregulates the expression of nerve elongation factors in normal human epidermal keratinocytes. J Dermatol Sci. 2018 Apr 23:S0923-1811(18)30186-5. [Content Brief]
[3]. Tanizaki H, et al. Oral administration of bepotastine besilate suppressed scratching behavior of atopic dermatitis model NC/Nga mice. Int Arch Allergy Immunol. 2008;145(4):277-82. [Content Brief]
[4]. Jon I Williams, et al. Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate. Curr Med Res Opin. 2010 Oct;26(10):2329-38. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bepotastine tosylate Related Classifications
HY-I0021A Related Classifications
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